1. Field of the Invention
The present invention relates to a benzoxazepine derivative having the formula: ##STR2## wherein A and B are both carbonyl groups, or one thereof represents a methylene group and the other a carbonyl group, R represents an aromatic group or a heterocyclic group which may be substituted, X represents a hydrogen atom, a halogen atom, preferably chlorine, bromine, fluorine, a C.sub.1 -C.sub.5 lower alkyl group, preferably a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.5 lower alkoxy group, preferably a C.sub.1 -C.sub.3 alkoxy group, a C.sub.7 -C.sub.9 arylalkoxy group, preferably a phenylalkoxy group, a hydroxyl group, a nitro group, or an ester group, and n is an integer of 2 to 10, preferably 2 to 8, more preferably 2 to 5, and salts thereof, and to a psycotropic composition containing the same as an active ingredient as well as the intermediate compounds for the preparation of the compound (I).
The novel benzoxazepine derivative having formula (I) of the present invention and its salts have a potent affinity for a serotonin receptor and an anticonflict activity, and are useful as drugs for psychotic disorders such as anxiety neurosis, phobic disorder, obsessive-compulsive disorder, psychosomatic disorder, post traumatic stress disorder, depressive neurosis, and as therapeutic drugs for diseases related to serotonergic neuron system, for example, eating disorder, climacteric disorder, and infantile autism.
2. Description of the Related Art
In the prior art, benzodiazepine type drugs, antipsychotic drugs and antidepressant drugs, are used as a therapeutic, for an anxiety neurosis, phobia, and obsessive-compulsive neurosis, but these drugs each have a problem with regard to the efficacy and side effects thereof.
Particularly, benzodiazepine type drugs are primarily used for an anxiety neurosis, but since a hypnotic action, muscle relaxing action, and a continuing dependence occur, there is an urgent need for the development of specific antianxiety drugs that do not have these side effects.
Various attempts have been made to solve these problems, and as a result, drugs having a selective affinity for a 5HT.sub.1A subtype considered probably useful as antianxiety drugs with little side effects. Namely, buspirone, gepirone, ipsapirone and the like have been or are being developed. ##STR3##
The above-mentioned buspirone, gepirone, and ipsapirone can partially alleviate various side effects, compared with benzodiazapine type drugs of the prior art, but can not be considered absolutely satisfactory, and there is a strong demand for antianxiety drugs having a high specificity with less side effects.